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/ Calcium Channel / Lercanidipine HCl

盐酸乐卡地平 /Lercanidipine HCl {[allProObj[0].p_purity_real_show]}

货号：A152276 同义名： 乐卡地平盐酸盐 / Lercanidipine (hydrochloride);Lercanidipine hydrochloride

Lercanidipine HCl是一种 L 型钙通道拮抗剂，用于治疗高血压。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Lercanidipine HCl 化学结构 CAS号：132866-11-6
Lercanidipine HCl 化学结构
CAS号：132866-11-6
Lercanidipine HCl 3D分子结构
CAS号：132866-11-6
Lercanidipine HCl 化学结构 CAS号：132866-11-6
Lercanidipine HCl 3D分子结构 CAS号：132866-11-6
规格 价格 会员价 库存 数量
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Lercanidipine HCl 纯度/质量文件 产品仅供科研

货号：A152276 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Ca2+ channel-like protein ↓ Calcium Channel ↓ Cav 2.2 ↓ 其他靶点 纯度
CDC25B-IN-2 ✔ Akt 99%+
Clevidipine ✔ 97%
Verapamil HCl ✔ 99%
Amlodipine ✔ 99%
Amlodipine maleate ✔ 98%
(+)-cis-Diltiazem HCl ✔ 95%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

 		99%+
Tanshinone IIA sulfonate sodium ✔ 98%
Ulixacaltamide ++

hCaV3.1, IC50: 50 nM

hCaV3.2, IC50: 110 nM

 		99%+
Dronedarone Hydrochloride ✔ 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

 		98%
Efonidipine HCl monoethanolate ✔ 98%
Cinnarizine ✔ 98%
SEA0400 ++

NCX, IC50: 33 nM

 		p38 MAPK,ROS,ERK 99%+
Fasudil HCl ✔ PKA,Rho 98%
ML-9 ✔ Akt,MLCK 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

 		95%
Lomerizine 2HCl ✔ 98%
Efonidipine ✔ 98%
Levamlodipine ✔ 97%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

 		97%
Isradipine ✔ 98%
Lacidipine ✔ 98%
Lercanidipine ✔ 98%
Loureirin B ✔ Potassium Channel 99%+
Tetracaine HCl ✔ 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

 		98%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

 		98%
Nicardipine ✔ 98%
Wilforgine ✔ 98+%
Econazole ✔ 99%+
Ginsenoside Rd ✔ NF-κB 98%
Fendiline HCl ✔ 98+%
Mesaconitine ✔ 98%
Tetrandrine ✔ 95%
Nifedipine ✔ 95%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

 		98%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

 		95+%
Azelnidipine ✔ 97%
Levetiracetam ✔ 98%
Nimodipine ✔ 95%
Benidipine HCl ✔ 98%
Pinaverium bromide ✔ 98%
Pranidipine ✔ 98%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

 		98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

 		97%
Cilnidipine ✔ 98%
Cinepazide Maleate ✔ 98%
Terfenadine ✔ 98%
YM-58483 ✔ 99%+
Ranolazine ✔ 98%
Praeruptorin A ✔ Akt,p38 MAPK 98%
Ranolazine 2HCl ✔ 98%
Felodipine ++++

L-type calcium channel, IC50: 0.15 nM

 		98%
PD173212 +++

N-type Ca2+ channel, IC50: 36 nM

 		98%
Levamlodipine besylate ✔ 97%
Carboxyamidotriazole Orotate ✔ 98%
IGS-1.76 ✔ 98+%
WH-4-023 ++++

Cav 2.2, IC50: 0.001 μM

 		++++

Cav 2.2, IC50: 0.001 μM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Lercanidipine HCl 生物活性

描述 Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. However, nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension[3]. Lercanidipine is a lipophilic third-generation DHP-CCB (Dihydropyridine-Calcium channel blocker), characterized by high vascular selectivity and persistence in the smooth muscle cell membranes. Lercanidipine prevents renal damage induced by angiotensin II and demonstrates anti-inflammatory, antioxidant, and anti-atherogenic properties through an increasing bioavailability of endothelial nitric oxide. It is associated with a regression of microvascular structural modifications in hypertensive patients. Lercanidipine produces a sustained blood pressure-lowering activity with a high rate of responder/normalized patients, associated with a favorable tolerability profile[4]. Lercanidipine and lercanidipine/enalapril for stage 1 or 2 hypertension highly improves office SBP and DBP, overall 24-hour BP (blood pressure), daytime BP, and nighttime BP, also reducing BPV (BP variability) with few adverse effects[5]. Lercanidipine was associated with a lower risk of peripheral edema and a lower risk of treatment withdrawal because of peripheral edema than were the first-generation, but not the second-generation, dihydropyridine CCBs[6].

Lercanidipine HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00741585 Essential Hypertension ... 展开 >> Cardiovascular Disease Stroke Chronic Kidney Disease 收起 << Phase 4 Completed - Spain ... 展开 >> CS Friol Friol, Lugo, Spain, 27220 CS Baiona Baiona, Pontevedra, Spain, 36300 CS Bueu Bueu, Pontevedra, Spain, 36930 CS A Estrada La Estrada, Pontevedra, Spain, 26680 CS A Guarda La Guardia, Pontevedra, Spain, 36780 CS Valmiñor Nigran, Pontevedra, Spain, 36250 CS Panxón Nigrán, Pontevedra, Spain, 36340 CS Tomiño Tomiño, Pontevedra, Spain, 36200 Bioengineering & Chronobilogy Labs., University of Vigo Vigo, Pontevedra, Spain, 36200 Hospital do Meixoeiro Vigo, Pontevedra, Spain, 36200 CS Calle Cuba Vigo, Pontevedra, Spain, 36202 CS A Doblada Vigo, Pontevedra, Spain, 36205 CS Coia Vigo, Pontevedra, Spain, 36209 CS Sardoma Vigo, Pontevedra, Spain, 36214 CS Teis Vigo, Pontevedra, Spain, 36216 CS Vilaboa Vilaboa, Pontevedra, Spain, 36141 CS San Roque Vilagarcía De Arousa, Pontevedra, Spain, 36600 CS Fingoi Lugo, Spain, 27002 Complexo Hospitalario Universitario de Ourense Orense, Spain, 32005 CS Lerez Pontevedra, Spain, 36156 收起 <<
NCT01180413 Essential Hypertension ... 展开 >> High Blood Pressure 收起 << Phase 4 Completed - Denmark ... 展开 >> Aarhus University Hospital - dept. cardiology (A) Aarhus, Denmark, 8000 收起 <<
NCT00424801 Microvascular Angina ... 展开 >> Hypertension 收起 << Not Applicable Terminated(Due to recent findi... 展开 >>ngs relating MRI contrast to nephrogenic systemic fibrosis) 收起 << December 2008 Denmark ... 展开 >> Aarhus Hospital Aarhus, Denmark, 8000 收起 <<

Lercanidipine HCl 参考文献

[1]Tawakkol S M, Farouk M, et al. Stability Study of the Calcium Channel Blocker Lercanidipine and its Determination by Reversed Phase Chromatography in Pharmaceutical Formulation and Plasma[J] . Analytical Chemistry Letters, 2014, 4(4):255-266.

[2]Canavesi M, Baldini N, et al. In vitro inhibitory effect of lercanidipine on cholesterol accumulation and matrix metalloproteinases secretion by macrophages. J Cardiovasc Pharmacol. 2004 Oct;44(4):416-22.

[3]Ranpise NS, Korabu SS, Ghodake VN. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride. Colloids Surf B Biointerfaces. 2014; 116:81‐87

[4]Grassi G, Robles NR, Seravalle G, Fici F. Lercanidipine in the Management of Hypertension: An Update. J Pharmacol Pharmacother. 2017; 8(4):155‐165

[5]Rayner B. The effect of lercanidipine or lercanidipine/enalapril combination on blood pressure in treatment-naïve patients with stage 1 or 2 systolic hypertension. Pragmat Obs Res. 2019;10:9‐14. Published 2019 Jan 22

[6]Makarounas-Kirchmann K, Glover-Koudounas S, Ferrari P. Results of a meta-analysis comparing the tolerability of lercanidipine and other dihydropyridine calcium channel blockers [published correction appears in Clin Ther. 2010 Feb;32(2):401-2]. Clin Ther. 2009; 31(8):1652‐1663

Lercanidipine HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.54mL

0.31mL

0.15mL

7.71mL

1.54mL

0.77mL

15.43mL

3.09mL

1.54mL

Lercanidipine HCl 技术信息

CAS号132866-11-6
分子式C36H42ClN3O6
分子量 648.188
别名 乐卡地平盐酸盐 ;Lercanidipine (hydrochloride);Lercanidipine hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C
溶解度

DMSO: 50 mg/mL(77.14 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Lercanidipine | 132866-11-6 | Membrane Transporter/Ion Channel | Neuronal Signaling | Apoptosis | Immunology/Inflammation | NF-κB | Metabolic Enzyme/Protease | MAPK/ERK Pathway | Calcium Channel | Apoptosis | Reactive Oxygen Species | p38 MAPK | NF-κB | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Lercanidipine HCl 纯度/质量文件 | Lercanidipine HCl 亚型比较 | Lercanidipine HCl 生物活性 | Lercanidipine HCl 临床数据 | Lercanidipine HCl 参考文献 | Lercanidipine HCl 实验方案 | Lercanidipine HCl 技术信息

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